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Method for preparing targeted anti-cancer medicament supported PLGA (poly(lactic-co-glycolic) acid) microparticles

An anti-cancer drug and micro-particle technology, applied in the field of preparation of PLGA micro-particles, can solve the problem of limited solubility of gemcitabine, improve the adhesion of urothelial cells, improve the anti-proliferative and anti-metabolic effects, and improve the cytotoxicity Effect

Inactive Publication Date: 2014-02-26
WUXI ZHONGKE GUANGYUAN BIOMATERIALS
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Problems solved by technology

However, after conversion to lipophilic derivatives, gemcitabine has very limited solubility in aqueous environments

Method used

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Embodiment Construction

[0009] In order to deepen the understanding of the present invention, the present invention is described in further detail below in conjunction with specific examples:

[0010] (1) 4-(N) Stearoyl Derivative (GEM-C 18 ) synthesis and separation: 100mg stearic acid, 119ul (0.5mmol) tributylamine were dissolved in 5ml tetrahydrofuran and cooled to -10°C, 65ul (0.5mmol) isobutyl chloroformic acid was dissolved in 5ml tetrahydrofuran, the It was added dropwise to the above cooled solution, and the reaction mixture was stirred under nitrogen for 30 min; gemcitabine (148 mg, 0.5 mmol) and thiobarbituric acid (TBA) (119 μl, 0.5 mmol) in 5 ml of anhydrous DMF were added. The solution was added carefully, and the mixture was stirred at room temperature for 36 h. After the acylation was completed, the excess solvent was evaporated, and the residue was dissolved in 10 mL of a mixed solvent of dichloromethane and ethanol (94 / 6, V / V); the mixture was centrifuged and suspended The liquid wa...

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Abstract

The invention relates to a method for preparing targeted anti-cancer medicament supported PLGA (poly(lactic-co-glycolic) acid) microparticles. According to the method, gemcitabine is transformed into 4-(N) stearoyl derivative (GEM-C18), and can be compounded into PLGA microparticles more stably and more uniformly, and the pharmaceutical activity of gemcitabine in cells can not be weakened; adhesion, anti-proliferation and anti-metabolism effects of fluorescent labeled GEM-C18-PLGA microparticles on urinary tract epithelium of non-malignant cancer (SV-HUC-1), low-grade or high-grade cancers (5673, HT-1376) can be remarkably improved. The product has a clinical application prospect in the field of targeted cancer cell killing and cancer treatment.

Description

technical field [0001] The invention relates to the preparation of a PLGA microparticle, in particular to the preparation of a PLGA microparticle loaded with an anticancer drug gemcitabine that can be used for targeted therapy. Background technique [0002] According to the epidemiological trend warning, bladder cancer is a serious medical condition. Intravesical instillation can make the drug enter the treatment site well, but the bioavailability of urothelial cells to the drug in intravesical infusion therapy is low, and due to the patient's compliance and practicality, a single intravesical infusion therapy is difficult to achieve. The maximum time is limited to 120min. Various advanced strategies such as novel APIs and device-assisted approaches can be used to optimize drug exposure. [0003] The nucleoside analog gemcitabine, due to its spectral antitumor activity and good safety profile, is used as a new generation of chemotherapy, gemcitabine itself as a prodrug, wh...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/48A61K31/7068A61P35/00A61K47/59
Inventor 韩志超许杉杉佴刚
Owner WUXI ZHONGKE GUANGYUAN BIOMATERIALS
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